An EP4 receptor antagonist
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ASP7657

Item No. 28578

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-[[[[1-(2-quinolinylmethyl)-5-(trifluoromethyl)-1H-indol-7-yl]carbonyl]amino]methyl]-cyclohexanecarboxylic acid
CAS Number
1196045-28-9
Molecular Formula
C28H26F3N3O3
Formula Weight
509.5
Purity
≥95% (mixture of isomers)
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16.5mg/mLDMSO: 16.5mg/mLDMSO:PBS (pH 7.2) (1:3): 0.25mg/mLEthanol: 12.5mg/mL
λmax
234 nm
SMILES
OC([C@H]1CC[C@H](CNC(C2=C(N(CC3=NC(C=CC=C4)=C4C=C3)C=C5)C5=CC(C(F)(F)F)=C2)=O)CC1)=O
InChi Code
InChI=1S/C28H26F3N3O3/c29-28(30,31)21-13-20-11-12-34(16-22-10-9-18-3-1-2-4-24(18)33-22)25(20)23(14-21)26(35)32-15-17-5-7-19(8-6-17)27(36)37/h1-4,9-14,17,19H,5-8,15-16H2,(H,32,35)(H,36,37)/t17-,19-
InChi Key
HBDTYYZZYCVTIJ-UAPYVXQJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $333

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    10 mg

    $589

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    25 mg

    $1,286

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    Product Description

    ASP7657 is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 (Kis = 2.21 and 6.02 nM for the human and rat receptors, respectively).1 It is selective for these receptors over the rat EP1, EP2, and EP3 receptors (IC50s = >1,000 nM for all), as well as a panel of 42 additional receptors and ion channels (IC50s = >1,000 nM for all). ASP7657 inhibits increases in cAMP accumulation induced by PGE2 in Jurkat cells expressing human EP4 and CHO cells expressing the rat receptor with IC50 values of 0.29 and 0.86 nM, respectively. It inhibits PGE2-induced decreases in LPS-stimulated TNF-α release in isolated rat whole blood in a dose-dependent manner. AP7657 (0.01 and 0.1 mg/kg per day) decreases albuminuria in the db/db mouse model of type 2 diabetes.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mizukami, K., Kamada, H., Yoshida, H., et al. Pharmacological properties of ASP7657, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Naunyn Schmiedebergs Arch. Pharmacol. 391(12), 1319-1326 (2018).